The pharmacokinetic and pharmacodynamic effects of single doses of parenterally administered opiates (heroin, morphine, hydromorphone, codeine, oxycodone, oxymorphone and sublingual buprenorphine) were studied. Concentrations of drug in blood and saliva levels were compared to pharmacologic effects. Additionally, the study was performed to determine if a metabolic marker for heroin abuse could be found in urine and other biological fluids. The subjects were healthy males with a history of heroin abuse. Informed consent was obtained and all procedures were approved by the hospital Institutional Review Board. A total of three test doses (placebo and two active doses) were administered in random order. Test measures were made for 24 hours and biological fluids were collected for 7 days after each test. The biological fluids were analyzed for drug and metabolites by chromatographic and immunoassay techniques. The significance of this study lies in the characterization of drug and metabolites appearance and disappearance over time and their relationship to drug-induced effects. Also, this continues our search for metabolite markers for heroin and other opiates in urine, saliva and other biological samples.